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    • 2. 发明公开
    • 시클로스포린계 약학적 조성물
    • 含有CYPOSPORIN和聚氧乙烯/聚氧乙烯嵌段共聚物的口服制剂的药物制剂,能够提供主要成分减少需要连续检查个体等离子体水平持续控制剂量的大量恒定剂和可渗透性血浆水平
    • KR1020040055669A
    • 2004-06-26
    • KR1020030093530
    • 2003-12-19
    • 폴리켐 에스.아.
    • 레고라,미첼라마일란드,페데리코
    • A61K38/13
    • A61K38/13A61K9/1075A61K9/4858A61K9/4866
    • PURPOSE: An orally administrable pharmaceutical formulation containing cyclosporin, ethanol, polyoxyethylene/polyoxypropylene block copolymers, water, solubilizers and an ester of C1-6 alkyl alcohol and C14-18 saturated fatty acid is provided. It is equal in biological properties to other formulations containing cyclosporin and can provide substantially constant and foreseeable plasma levels of the active ingredient thus reducing the need to continuously check the plasma levels of individuals to continuously control the dosage amount. CONSTITUTION: The pharmaceutical formulation for the oral administration of cyclosporin contains: (a) 8 to 12% by weight of cyclosporin; (b) 12 to 18% by weight of ethanol; (c) 8 to 12% by weight of a polyoxyethylene/polyoxypropylene block copolymer; (d) 4 to 6% by weight of water; (e) 28 to 40% by weight of solubilizers having a HLB from 13 to 15; and (f) 20 to 30% by weight of an ester of a C1-6 alkyl alcohol and a C14-18 saturated fatty acid, based on the total weight of the formulation. The cyclosporin is cyclosporin A, the solubilizers are caprylocaproyl macrogol-8-glyceride, the ester of C1-6 alkyl alcohol and C14-18 saturated fatty acid is isopropyl myristate.
    • 目的:提供含有环孢菌素,乙醇,聚氧乙烯/聚氧丙烯嵌段共聚物,水,增溶剂和C 1-6烷基醇和C 14-18饱和脂肪酸酯的口服给药药物制剂。 其生物学性质与含有环孢菌素的其它制剂相同,并且可以提供活性成分的基本恒定和可预见的血浆水平,从而减少连续检查个体血浆水平以持续控制剂量的需要。 构成:口服环孢菌素的药物制剂含有:(a)8-12重量%的环孢菌素; (b)12至18重量%的乙醇; (c)8〜12重量%的聚氧乙烯/聚氧丙烯嵌段共聚物; (d)4至6重量%的水; (e)28至40重量%的HLB为13至15的增溶剂; 和(f)20至30重量%的基于制剂总重量的C 1-6烷基醇和C 14-18饱和脂肪酸的酯。 环孢菌素为环孢菌素A,增溶剂为辛酰己酰甘醇-8-甘油酯,C 1-6烷基醇和C 14-18饱和脂肪酸的酯为肉豆蔻酸异丙酯。